Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM[1].
TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain[1].
Hythiemoside B is isolated as a white amorphous powder. Hythiemoside B is an ent-pimarane glucoside isolated from the aerial part of Siegesbecikia orientalis L. (Asteraceae)[1].
Thymopoietin i/ii (29-41) (bovine) is a peptide corresponding to positions 29-41 of bovine thymopoietin II. Thymopoietin i/ii (29-41) (bovine) is a neuromuscular blocker[1].
Penpulimab is an IgG1 backbone anti-PD-1 monoclonal antibody with antitumor activities[1].
ODN 105871, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105871 can be uesd for inflammatory immune responses research[1].
KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). IC50 value:Target: KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cell.
(S)-2-((S)-2-Amino-3-phenylpropanamido)-3-methylbutanoic acid is a valine derivative[1].
Fenbendazole is a broad spectrum benzimidazole anthelmintic used against gastrointestinal parasites.Target: AntiparasiticFenbendazole is a broad spectrum benzimidazole anthelmintic used against gastrointestinal parasites including: giardia, roundworms, hookworms, whipworms, the taenia species of tapeworms(It is effective against the Taenia species of tapeworm but not against the common tapeworm, Dipylidium caninum.), pinworms, aelurostrongylus, paragonimiasis, strongyles and strongyloides and can be administered to sheep, cattle, horses, fish, dogs, cats, rabbits and seals. Drug interactions may occur if using bromsalan flukicides such as dibromsalan and tribromsalan. Abortions in cattle and death in sheep have been reported after using these medications together. Fenbendazole is poorly absorbed from the gastrointestinal tract in most species. The LD50 in laboratory animals exceeds 10 g/kg when administered orally. From Wikipedia.
E3 ligase Ligand-Linker Conjugates 16 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells[1].
JTP-117968, a novel selective glucocorticoid receptor modulator (a non-steroidal SGRM, IC50 of 6.8 nM), exhibits improved transrepression/transactivation dissociation[1].
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].
Aminooxy-PEG1-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Methacycline HCl is a tetracycline antibiotic.Target: Antibacterial Methacycline HCl is a broad-spectrum semisynthetic antibiotic related to tetracycline but excreted more slowly and maintaining effective blood levels for a more extended period.
Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood.IC50:0.44 nM(PGD2-induced eosinophil shape change)Kd value:1.1nM(CRTh2 receptor)[1]In vitro: CRTh2-mediated shape change in eosinophils was used to profile QAW039 in whole blood and represents a physiologically relevant environment. The comparable IC50 values for QAW039 in the whole blood and isolated shape-change assays are consistent with its lower plasma-protein binding and its relatively slow dissociation kinetics that drive its increased potency .QAW039 is highly potent in whole-blood systems, with the IC50 value obtained consistent with the affinity values calculated from radioligand experiments. In a further disease-relevant cellular context, the potency of QAW039 in the isolated Th2 cell cytokine inhibition assay is consistent with its CRTh2 receptor affinity, and, as with eosinophil assay readouts, this represents an improved potency compared with QAV680[2].
Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM[1].
6,4'-Dihydroxy-7-methoxyflavanone, a flavonoid, is a nature product that could be isolated from Heartwood Dalbergia odorifera. 6,4'-Dihydroxy-7-methoxyflavanone inhibits receptor activators of nuclear factor kappa-B ligand (RANKL) induced osteoclastogenesis. 6,4'-Dihydroxy-7-methoxyflavanone has antioxidant, anti-inflammatory and neuroprotective effects. 6,4'-Dihydroxy-7-methoxyflavanone can be used in research of osteoporosis[1].
THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe[1].
CMPD167 (MRK-1) is an orally acitve small molecule that binds to CCR5 to inhibit gp120 association, inhibits different stages of the virus-cell attachment and entry process (CCR5-using virus SHIV-162P3, IC50<1 nM).
3′-Methoxydaidzin is a flavonoid compound isolated from the leaves of Ilex cornuta Lindl ex Paxt[1].
GSK 3008348 (hydrochloride) is a small molecule integrin αvβ6 antagonist, extracted from patent WO/2014154725A1, example 1. The affinity (pIC50) for the human - a 6 protein in the Fluorescence Polarisation Assay for GSK 3008348 (hydrochloride) is 8.1, whereas its affinity in the cell Adhesion Assays was for: ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC50 = 6.9); ανβ8 (pIC50 = 7.7).
Lecirelin is a synthetic gonadotropin-releasing hormone (GnRH) analogue. Lecirelin is widely used for the research of bovine ovarian follicular cysts[1].
RSV-IN-2 is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins (wild-type, EC50 = 0.27 nM; D486N-mutant, EC50 = 0.70 nM).
K-Ras-IN-2 (Compound CHI-000-667) is a K-Ras antagonist, and can be used for tumor research[1].
Sinapine is an alkaloid from seeds of the cruciferous species which shows favorable biological activities such as antioxidant and radio-protective activities.
Fmoc-Thr(GalNAc(Ac)3-β-D)-OH inhibits cancer cell growth, through targeting intricate cancer-specific pathways while simultaneously strengthening immunologic response[1].
Antitubercular agent-9 shows effective antitubercular activity with a MIC value of 1.03-2.32 μM.
Boc-Cys(tBu)-OH is a cysteine derivative[1].
Capreomycin is a peptide antibiotic, commonly grouped with the aminoglycosides, which is given in combination with other antibiotics for MDR-tuberculosis.IC50 value:Target: The drug should not be given with streptomycin or other drugs that may damage the auditory vestibular nerve. Patients on this drug will often require audiology tests. It is a cyclic peptide.Capreomycin is administered intramuscularly and shows bacteriostatic activity.